JP7222909B2 - （ｓ）－アフォキソラネルの結晶形 - Google Patents

（ｓ）－アフォキソラネルの結晶形 Download PDF

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Publication number
JP7222909B2
JP7222909B2 JP2019554802A JP2019554802A JP7222909B2 JP 7222909 B2 JP7222909 B2 JP 7222909B2 JP 2019554802 A JP2019554802 A JP 2019554802A JP 2019554802 A JP2019554802 A JP 2019554802A JP 7222909 B2 JP7222909 B2 JP 7222909B2
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Prior art keywords
compound
formula
afoxolaner
solvent
crystalline
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JP2019554802A
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Japanese (ja)
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JP2020513010A (ja
Inventor
デ フリース レーロフ ヨハンネス ゴーター
ブリュノ バイヨン
シルヴェーヌ ラフォン
ド サン ミシェル ミリアン ゲイ
ステファーヌ コズロヴィツェ
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Boehringer Ingelheim Animal Health USA Inc
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Boehringer Ingelheim Animal Health USA Inc
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42—Oxazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
    • C07D261/04—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/10—Anthelmintics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07—Optical isomers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Liquid Crystal Substances (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pyridine Compounds (AREA)
  • Heterocyclic Compounds That Contain Two Or More Ring Oxygen Atoms (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Secondary Cells (AREA)
JP2019554802A 2017-04-05 2018-04-05 （ｓ）－アフォキソラネルの結晶形 Active JP7222909B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201762482175P 2017-04-05 2017-04-05
US62/482,175 2017-04-05
PCT/US2018/026328 WO2018187623A1 (en) 2017-04-05 2018-04-05 Crystalline forms of (s)-afoxolaner

Publications (2)

Publication Number Publication Date
JP2020513010A JP2020513010A (ja) 2020-04-30
JP7222909B2 true JP7222909B2 (ja) 2023-02-15

Family

ID=62092252

Family Applications (1)

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JP2019554802A Active JP7222909B2 (ja) 2017-04-05 2018-04-05 （ｓ）－アフォキソラネルの結晶形

Country Status (22)

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US (2) US10662163B2 (ko)
EP (1) EP3606911A1 (ko)
JP (1) JP7222909B2 (ko)
KR (1) KR102612648B1 (ko)
CN (2) CN120172925A (ko)
AR (1) AR111412A1 (ko)
AU (1) AU2018250304B2 (ko)
CA (1) CA3059114A1 (ko)
CL (1) CL2019002840A1 (ko)
CO (1) CO2019011980A2 (ko)
EA (1) EA201992360A1 (ko)
IL (1) IL269792B (ko)
MD (1) MD20190080A2 (ko)
MX (1) MX2019011931A (ko)
MY (1) MY188420A (ko)
PH (1) PH12019502277A1 (ko)
SG (1) SG11201909229SA (ko)
TW (1) TWI782976B (ko)
UA (1) UA125727C2 (ko)
UY (2) UY37665A (ko)
WO (1) WO2018187623A1 (ko)
ZA (1) ZA201906464B (ko)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2018187623A1 (en) * 2017-04-05 2018-10-11 Merial, Inc. Crystalline forms of (s)-afoxolaner
WO2021254445A1 (zh) * 2020-06-19 2021-12-23 东莞市东阳光仿制药研发有限公司 一种gaba抑制剂的晶型及其制备方法
KR20230043904A (ko) 2020-07-24 2023-03-31 엘랑코 유에스 인코포레이티드 이속사졸린 화합물 및 이의 중간체의 제조 공정
CN116744917A (zh) 2020-09-04 2023-09-12 礼蓝美国公司 适口调配物
CN117486869A (zh) * 2023-11-06 2024-02-02 北京康立生医药技术开发有限公司 一种眼科治疗药物新的制备方法
CN118536571B (zh) * 2024-05-31 2025-02-25 北京无问芯穹科技有限公司 一种构建扩散变换器模型的方法、系统、设备及存储介质
WO2025257633A1 (en) 2024-06-12 2025-12-18 Boehringer Ingelheim Vetmedica Gmbh Long-acting castor oil-containing injectable formulations and methods of use thereof

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2010536767A (ja) 2007-08-17 2010-12-02 イー・アイ・デュポン・ドウ・ヌムール・アンド・カンパニー ５−ハロアルキル−４，５−ジヒドロイソキサゾール誘導体を調製する方法
JP2013528177A (ja) 2010-05-27 2013-07-08 イー・アイ・デュポン・ドウ・ヌムール・アンド・カンパニー ４−［５−［３−クロロ−５−（トリフルオロメチル）フェニル］−４，５−ジヒドロ−５−（トリフルオロメチル）−３−イソオキサゾリル］−ｎ−［２−オキソ−２−［（２，２，２−トリフルオロエチル）アミノ］エチル］−１−ナフタレンカルボキサミドの結晶質形態
WO2016138339A1 (en) 2015-02-26 2016-09-01 Merial, Inc. Long-acting injectable formulations comprising an isoxazoline active agent, methods and uses thereof

Family Cites Families (8)

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TWI412322B (zh) 2005-12-30 2013-10-21 Du Pont 控制無脊椎害蟲之異唑啉
TWI430995B (zh) * 2007-06-26 2014-03-21 Du Pont 萘異唑啉無脊椎有害動物控制劑
RS58417B1 (sr) * 2011-09-12 2019-04-30 Merial Inc Paraziticidne kompozicije koje sadrže izoksazolinsko aktivno sredstvo, postupci i upotrebe povezane sa njima
WO2014090918A1 (en) * 2012-12-13 2014-06-19 Novartis Ag Process for the enantiomeric enrichment of diaryloxazoline derivatives
JP2015028006A (ja) * 2013-06-27 2015-02-12 日産化学工業株式会社 イソキサゾリン化合物の結晶性多形体およびその製造方法
SG11201708068PA (en) * 2015-04-08 2017-10-30 Merial Inc Extended release injectable formulations comprising an isoxazoline active agent, methods and uses thereof
ES2903286T3 (es) 2016-04-06 2022-03-31 Boehringer Ingelheim Animal Health Usa Inc Proceso de preparación de compuestos de isoxazolina enriquecidos enantioméricamente y de solvato de tolueno cristalino de (S)-afoxolaner
WO2018187623A1 (en) * 2017-04-05 2018-10-11 Merial, Inc. Crystalline forms of (s)-afoxolaner

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2010536767A (ja) 2007-08-17 2010-12-02 イー・アイ・デュポン・ドウ・ヌムール・アンド・カンパニー ５−ハロアルキル−４，５−ジヒドロイソキサゾール誘導体を調製する方法
JP2013528177A (ja) 2010-05-27 2013-07-08 イー・アイ・デュポン・ドウ・ヌムール・アンド・カンパニー ４−［５−［３−クロロ−５−（トリフルオロメチル）フェニル］−４，５−ジヒドロ−５−（トリフルオロメチル）−３−イソオキサゾリル］−ｎ−［２−オキソ−２−［（２，２，２−トリフルオロエチル）アミノ］エチル］−１−ナフタレンカルボキサミドの結晶質形態
WO2016138339A1 (en) 2015-02-26 2016-09-01 Merial, Inc. Long-acting injectable formulations comprising an isoxazoline active agent, methods and uses thereof

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
小嶌隆史，医薬品開発における結晶性選択の効率化を目指して，薬剤学，2008年09月01日，Vol.68, No.5，p.344-349
平山令明，有機化合物結晶作製ハンドブック，2008年，pp.10-11,57-72,78-81
浅原 照三，溶剤ハンドブック，1985年，pp.47-51
芹澤一英，医薬品の多形現象と晶析の化学，2002年，p.273, 278, 305-317

Also Published As

Publication number Publication date
KR20190136055A (ko) 2019-12-09
CA3059114A1 (en) 2018-10-11
AU2018250304A1 (en) 2019-10-31
ZA201906464B (en) 2021-08-25
AR111412A1 (es) 2019-07-10
NZ757869A (en) 2024-11-29
EA201992360A1 (ru) 2020-09-02
EP3606911A1 (en) 2020-02-12
MX2019011931A (es) 2020-01-13
WO2018187623A1 (en) 2018-10-11
WO2018187623A8 (en) 2019-10-24
CL2019002840A1 (es) 2020-01-10
US20200270219A1 (en) 2020-08-27
IL269792A (en) 2019-11-28
JP2020513010A (ja) 2020-04-30
US20180354917A1 (en) 2018-12-13
BR112019021072A2 (pt) 2020-05-12
KR102612648B1 (ko) 2023-12-11
SG11201909229SA (en) 2019-11-28
CN111032634A (zh) 2020-04-17
CN120172925A (zh) 2025-06-20
CN111032634B (zh) 2025-04-11
US10662163B2 (en) 2020-05-26
UY40794A (es) 2024-07-15
MY188420A (en) 2021-12-08
TW201841895A (zh) 2018-12-01
CO2019011980A2 (es) 2020-02-18
UY37665A (es) 2018-10-31
UA125727C2 (uk) 2022-05-25
AU2018250304B2 (en) 2022-03-03
US11130739B2 (en) 2021-09-28
PH12019502277A1 (en) 2020-09-14
TWI782976B (zh) 2022-11-11
MD20190080A2 (ro) 2020-04-30
IL269792B (en) 2022-04-01

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